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公开(公告)号：EP3220910B1
公开(公告)日：2020-01-15
申请号：EP15861650.8
申请日：2015-11-13
Applicant: Merck Sharp & Dohme Corp.
Inventor： KUANG, Rongze , TING, Pauline , ALI, Amjad , WU, Heping , BERLIN, Michael , STAMFORD, Andrew , WANG, Hongwu , ZHOU, Gang , KIM, David , DENG, Qiaolin , LIM, Yeon-Hee , YU, Younong
IPC: A61K31/497 , C07D241/26 , C07D413/04
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公开(公告)号：EP3038466B1
公开(公告)日：2018-05-23
申请号：EP14840648.1
申请日：2014-08-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： ALI, Amjad , GALLO, Gioconda, V. , HENDERSON, Timothy, J. , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , METZGER, Edward , RUIZ, Manuel de Lera , STAMFORD, Andrew , TEMPEST, Paul , WHITEHEAD, Brent , WU, Heping
IPC: C07D519/00 , C07D491/147 , A61K31/519 , A61P25/00 , A61P25/16 , A61P25/28
CPC classification number: C07D519/00 , C07D491/147
Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
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公开(公告)号：EP3220910A1
公开(公告)日：2017-09-27
申请号：EP15861650.8
申请日：2015-11-13
Applicant: Merck Sharp & Dohme Corp.
Inventor： KUANG, Rongze , TING, Pauline , ALI, Amjad , WU, Heping , BERLIN, Michael , STAMFORD, Andrew , WANG, Hongwu , ZHOU, Gang , KIM, David , DENG, Qiaolin , LIM, Yeon-Hee , YU, Younong
IPC: A61K31/497 , C07D241/26 , C07D413/04
Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
Abstract translation: 公开了式A和式A-1的化合物或其盐，以及包含这些化合物或其盐的药物制剂（药物组合物） 其中“R1”，“RA-1”，“R2”，“R3”和“Het”如上文所定义，认为该化合物适用于选择性拮抗A2a受体，例如以高密度 在基底神经节。 据信这样的化合物和药物制剂可用于治疗或控制神经退行性疾病，例如帕金森病，或由于使用用于治疗或控制帕金森病的某些药物引起的运动障碍。
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公开(公告)号：EP3377065A1
公开(公告)日：2018-09-26
申请号：EP16866885.3
申请日：2016-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： GRAHAM, Thomas, H. , YU, Tao , WADDELL, Sherman, T. , MCCAULEY, John, A. , STAMFORD, Andrew , LIU, Wensheng , GROBLER, Jay, A. , XU, Libo
IPC: A61K31/53 , A61K31/495 , A61K31/4985 , C07D295/00 , C07D401/02 , C07D403/02
CPC classification number: A61K31/675 , A61K31/426 , A61K31/513 , A61K31/52 , A61K2300/00 , A61P31/18 , C07D491/20 , C07F9/6561
Abstract: The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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5.发明授权
公开(公告)号：EP2382204B1
公开(公告)日：2018-07-11
申请号：EP09795879.7
申请日：2009-12-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： NEUSTADT, Bernard R. , STAMFORD, Andrew , HAO, Jinsong , JAYNE, Charles Lee , XIA, Yan
IPC: C07D498/08 , C07D471/08 , C07D401/14 , C07D401/12
CPC classification number: C07D401/14 , C07D401/12 , C07D471/08 , C07D498/08
Abstract: The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
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6.发明授权
公开(公告)号：EP2291358B1
公开(公告)日：2018-03-28
申请号：EP09747426.6
申请日：2009-05-13
Applicant: Merck Sharp & Dohme Corp.
IPC: C07D231/22 , C07D231/38 , A61K31/415
CPC classification number: C07D231/22 , C07D231/38
Abstract: The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
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7.发明授权HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS SUITABLE FOR TREATMENT OR PREVENTION OF CENTRAL NERVOUS SYSTEM DISORDERS 有权适用于治疗或预防中枢神经系统疾病的杂环基取代的[1,2,4]三唑并[1,5-C]喹唑啉-5-胺化合物
公开(公告)号：EP2945632B1
公开(公告)日：2018-03-07
申请号：EP13866588.0
申请日：2013-12-20
Applicant: Merck Sharp & Dohme Corp.
Inventor： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy, J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda, V. , WON, Walter , WU, Heping , DENG, Qiaolin
IPC: C07D487/04 , A61K31/4985 , A61K31/519 , A61P25/16
CPC classification number: C07D519/00 , C07D487/04
Abstract: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
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8.发明公开PIPERAZINE-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 有权哌嗪[1,2,4]三唑[1,5-C]喹唑啉-5-氨基 - 维生素M11A-ANTAGONISTISCHEN EIGENSCHAFTEN
公开(公告)号：EP2938344A1
公开(公告)日：2015-11-04
申请号：EP13867977.4
申请日：2013-12-20
Applicant: Merck Sharp & Dohme Corp.
Inventor： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , BERLIN, Michael , TING, Pauline , ZHOU, Gang , YU, Tao , BOYCE, Christopher , KELLY, Joseph Michael , TAGAT, Jayaram, R. , ZHENG, Junying , HUANG, Xianhai , ZHOU, Wei , KIM, Jae-Hun , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda, V. , WON, Walter , WU, Heping , ANAND, Rajan , DENG, Qiaolin
IPC: A61K31/4985 , A61K31/519
CPC classification number: C07D487/04 , C07D487/08 , C07D487/18 , C07D513/04
Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
Abstract translation: 公开了式A化合物：（结构上表示）其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。
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公开(公告)号：EP2350020B1
公开(公告)日：2014-08-13
申请号：EP09741076.5
申请日：2009-09-30
Applicant: Merck Sharp & Dohme Corp.
Inventor： STAMFORD, Andrew , MILLER, Michael, W. , DEMONG, Duane, Eugene , GREENLEE, William, J. , KOZLOWSKI, Joseph, A. , LAVEY, Brian, J. , WONG, Michael, K.C. , YU, Wensheng , DAI, Xing , YANG, De-Yi , ZHOU, Guowei
IPC: C07D235/02 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/12 , C07D491/10 , A61K31/4184 , A61K31/4188 , A61K31/4439 , A61K31/4453 , A61K31/47
CPC classification number: C07D235/02 , A61K31/4184 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/12 , C07D491/10 , A61K2300/00
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10.发明公开2-SPIRO-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE 有权2螺取代IMINOTHIAZINE及其单和二氧化AS BACE抑制剂，组合物及其
公开(公告)号：EP2747769A1
公开(公告)日：2014-07-02
申请号：EP12825781.3
申请日：2012-08-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： WU, Wen-Lian , BURNETT, Duane, A. , STAMFORD, Andrew , CUMMING, Jared, N. , ASBEROM, Theodros , BENNETT, Chad , SASISKUMAR, Thavalakulamgara, K. , SCOTT, Jack, D.
IPC: A61K31/547
CPC classification number: C07D417/14 , A61K45/06 , C07D279/34 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04 , C07D513/10 , C07D519/00
Abstract: In its many embodiments, the present invention provides provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of the variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
